Protein kinase G modulates human myocardial passive stiffness by phosphorylation of the titin springs

Circ Res. 2009 Jan 2;104(1):87-94. doi: 10.1161/CIRCRESAHA.108.184408. Epub 2008 Nov 20.

Abstract

The sarcomeric titin springs influence myocardial distensibility and passive stiffness. Titin isoform composition and protein kinase (PK)A-dependent titin phosphorylation are variables contributing to diastolic heart function. However, diastolic tone, relaxation speed, and left ventricular extensibility are also altered by PKG activation. We used back-phosphorylation assays to determine whether PKG can phosphorylate titin and affect titin-based stiffness in skinned myofibers and isolated myofibrils. PKG in the presence of 8-pCPT-cGMP (cGMP) phosphorylated the 2 main cardiac titin isoforms, N2BA and N2B, in human and canine left ventricles. In human myofibers/myofibrils dephosphorylated before mechanical analysis, passive stiffness dropped 10% to 20% on application of cGMP-PKG. Autoradiography and anti-phosphoserine blotting of recombinant human I-band titin domains established that PKG phosphorylates the N2-B and N2-A domains of titin. Using site-directed mutagenesis, serine residue S469 near the COOH terminus of the cardiac N2-B-unique sequence (N2-Bus) was identified as a PKG and PKA phosphorylation site. To address the mechanism of the PKG effect on titin stiffness, single-molecule atomic force microscopy force-extension experiments were performed on engineered N2-Bus-containing constructs. The presence of cGMP-PKG increased the bending rigidity of the N2-Bus to a degree that explained the overall PKG-mediated decrease in cardiomyofibrillar stiffness. Thus, the mechanically relevant site of PKG-induced titin phosphorylation is most likely in the N2-Bus; phosphorylation of other titin sites could affect protein-protein interactions. The results suggest that reducing titin stiffness by PKG-dependent phosphorylation of the N2-Bus can benefit diastolic function. Failing human hearts revealed a deficit for basal titin phosphorylation compared to donor hearts, which may contribute to diastolic dysfunction in heart failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Connectin
  • Consensus Sequence
  • Cyclic AMP-Dependent Protein Kinases / physiology
  • Cyclic GMP / physiology
  • Cyclic GMP-Dependent Protein Kinases / physiology*
  • Dogs
  • Elasticity
  • Heart Failure, Diastolic / metabolism*
  • Heart Ventricles / metabolism*
  • Humans
  • Molecular Sequence Data
  • Muscle Proteins / genetics
  • Muscle Proteins / metabolism*
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism
  • Myocytes, Cardiac / ultrastructure
  • Myofibrils / drug effects
  • Myofibrils / ultrastructure
  • Nitric Oxide / physiology
  • Phosphorylation
  • Protein Isoforms / metabolism
  • Protein Kinases / genetics
  • Protein Kinases / metabolism*
  • Protein Processing, Post-Translational*
  • Recombinant Fusion Proteins / physiology
  • Sarcomeres / metabolism
  • Sarcomeres / ultrastructure
  • Structure-Activity Relationship
  • Ventricular Remodeling / physiology

Substances

  • Connectin
  • Muscle Proteins
  • Protein Isoforms
  • Recombinant Fusion Proteins
  • TTN protein, human
  • Nitric Oxide
  • Protein Kinases
  • Cyclic AMP-Dependent Protein Kinases
  • Cyclic GMP-Dependent Protein Kinases
  • Cyclic GMP